货号	规格	价格	上海	北京	珠海	重庆	武汉
S86924-2mg买3赠1	98.80%	￥140.00 S86924-2mg ￥140.00 现货（买3赠1）	5 5	-	-	-	-
S86924-5mg买3赠1	98.80%	￥200.00 S86924-5mg ￥200.00 现货（买3赠1）	6 6	-	-	-	-
S86924-10mg买3赠1	98.80%	￥370.00 S86924-10mg ￥370.00 现货（买3赠1）	6 6	-	-	-	-
S86924-25mg促销	98.80%	￥580.00 ￥464.00 S86924-25mg ￥464.00 现货	6 6	-	-	-	-
S86924-50mg促销	98.80%	￥930.00 ￥744.00 S86924-50mg ￥744.00 现货	4 4	-	-	-	-
S86924-100mg促销	≥98%	￥1450.00 ￥1160.00 S86924-100mg ￥1160.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.

靶点：

p110α:5441 nM (IC50);p110β:3377 nM (IC50);p110δ:12.7 nM (IC50);p110γ:1389 nM (IC50);hVps34:12682 nM (IC50);DNA-PK:18749 nM (IC50);PI3K

体外研究：

Acalisib (GS-9820) is more selective for PI3Kδ (IC50=12.7 nM) relative to other PI3K class I enzymes (IC50: PI3Kα, 5,441 nM; PI3Kβ, 3,377 nM; PI3Kγ, 1,389 nM). Acalisib is also 103-fold more selective against PI3Kδ than against related kinases, such as PI3KCIIβ (IC50>10 nM), hVPS34 (IC50=12.7 μM), DNA-PK (IC50=18.7 μM), and mTOR (IC50>10 nM). In fibroblasts, the PDGF receptor signals through PI3Kα and the GPCR for lysophosphatidic acid (LPA) signals through PI3Kβ. Acalisib reduces PDGF-induced pAkt by only 50% at 11,585 nM, and LPA-induced pAkt by 50% at 2,069 nM

体内研究：

To dissect the relative contribution of PI3Kα and PI3Kδ inhibition in the reduction of obesity, obese hyperphagic ob/ob mice are treated with a selective PI3Kα inhibitor, BYL-719, or with a selective PI3Kδ inhibitor, Acalisib (GS-9820). Remarkably, BYL-719 reduces body weight after 15 days of treatment to a similar extent as CNIO-PI3Ki, whereas Acalisib has no significant effect at the same doses as BYL-719. It should be noted that 10 mg/kg of Acalisib is sufficient to reduce the growth of multiple myeloma xenografts in mice

参考文献：

1. Shugg RP, et al. Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption. J Biol Chem. 2013 Dec 6;288(49):35346-57. 2. Lopez-Guadamillas E, et al. PI3Kα inhibition reduces obesity in mice. Aging (Albany NY). 2016 Nov 4;8(11):2747-2753.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.491 ml	12.457 ml	24.913 ml
5 mM	0.498 ml	2.491 ml	4.983 ml
10 mM	0.249 ml	1.246 ml	2.491 ml
50 mM	0.05 ml	0.249 ml	0.498 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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